MEDICINAL CHEMISTRY APPLIED TO PROBLEMS PROMINENT IN SENESCENCE

药物化学应用于解决衰老中的突出问题

• 批准号: 3823134
• 负责人: J PITHA
• 金额: --
• 依托单位: NATIONAL INSTITUTE ON AGING
• 依托单位国家: 美国
• 资助国家: 美国
• 起止时间: 至
• 项目状态: 未结题
• 来源: https://reporter.nih.gov/project-details/3823134
• 关键词: antiadrenergic agents; beta antiadrenergic agent; drug adverse effect; drug design /synthesis /production; drug metabolism; drug screening /evaluation; drug vehicle; human subject; lipid solubility; nutrition related tag; peripheral nervous system; retinoids; water solubility

The work on ligands for receptors of catecholamines resulted in the preparation of compounds which selectively lesion either beta-adrenoceptors or alpha one-adrenoceptors. The lesion process in question leads to irreversible deactivation of receptors located on the cell surface through alkylation with a ligand; there is no cellular death or necrosis in the tissue. The potential of the approach was demonstrated by work on the peripheral nervous system (performed within the Section) and by work on the central nervous system (performed at The Johns Hopkins University). Lesions in the periphery of rats lasted for about a week and there was no crossover into the central nervous system. Lesions in beta-adrenoceptors in the brains of rats were long lasting (greater then 30 days) and by choice of conditions could be localized to the proximity of the injection site. The work on solubilizers resulted in the successful experimental therapy of hypervitaminosis A. Also, the first steps have been initiated by the licensing office of the Department of Commerce to bring the new pharmaceutical form of sex hormones, which is based on the solubilizers developed at NIA, into practical use.

对儿茶酚胺受体配体的研究导致了 选择性损害β-肾上腺素受体或 或α肾上腺素受体。 所讨论的病变过程导致 位于细胞表面的受体的不可逆失活， 与配体烷基化;在细胞中没有细胞死亡或坏死。 组织. 该方法的潜力已通过关于 周围神经系统（在该科内进行）和工作的 中枢神经系统（在约翰霍普金斯大学进行）。 大鼠外周的病变持续约一周， 进入中枢神经系统 β-肾上腺素受体病变 在大鼠大脑中的作用持续时间长（大于30天）， 条件的选择可以局限于注射附近 绝佳的价钱 增溶剂的工作导致了成功的实验治疗， 维生素A过多症 此外，第一批步骤已经由 商务部许可证办公室将新的 性激素的药物形式，其基于增溶剂 在NIA开发，投入实际使用。